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醋丁洛尔和双醋洛尔在人体中的血浆蛋白结合情况。

Blood plasma binding of acebutolol and diacetolol in man.

作者信息

Coombs T J, Coulson C J, Smith V J

出版信息

Br J Clin Pharmacol. 1980 Apr;9(4):395-7. doi: 10.1111/j.1365-2125.1980.tb01067.x.

DOI:10.1111/j.1365-2125.1980.tb01067.x
PMID:7378256
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1429991/
Abstract

1 Acebutolol or diacetolol were added to fresh human plasma in varying concentrations and their extent of binding at 25 degrees C measureed by an equilibrium dialysis technique. 2 The extent of binding for both compounds was shown to be very low, being 11-19% for acebutolol and 6-9% for diacetolol. 3 Partition coefficients were measured in an n- octanol/phosphate buffer (0.05M, pH 7.4) solvent system. For a cebutolol, P = 0.62 and for diacetol, P = 0.08. 4 The very low plasma binding is in accord with the hydrophilic partition coefficients of these compounds.

摘要
  1. 将醋丁洛尔或双醋洛尔以不同浓度添加到新鲜人血浆中,并通过平衡透析技术测定它们在25℃时的结合程度。2. 结果表明,两种化合物的结合程度都非常低,醋丁洛尔为11 - 19%,双醋洛尔为6 - 9%。3. 在正辛醇/磷酸盐缓冲液(0.05M,pH 7.4)溶剂系统中测量分配系数。醋丁洛尔的P = 0.62,双醋洛尔的P = 0.08。4. 极低的血浆结合与这些化合物的亲水性分配系数一致。

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引用本文的文献

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Acebutolol. A review of its pharmacological properties and therapeutic efficacy in hypertension, angina pectoris and arrhythmia.醋丁洛尔。其药理学特性及在高血压、心绞痛和心律失常治疗中的疗效综述。
Drugs. 1985 Jun;29(6):531-69. doi: 10.2165/00003495-198529060-00003.
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Clinical pharmacokinetics of beta-adrenoceptor antagonists. An update.β-肾上腺素能受体拮抗剂的临床药代动力学。最新进展。
Clin Pharmacokinet. 1987 May;12(5):305-20. doi: 10.2165/00003088-198712050-00001.
5
Effect of adjuvant arthritis on the disposition of acebutolol enantiomers in rats.佐剂性关节炎对大鼠醋丁洛尔对映体处置的影响。
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本文引用的文献

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Influence of binding on the toxicity of bilirubin.结合作用对胆红素毒性的影响。
Ann N Y Acad Sci. 1973 Nov 26;226:225-37. doi: 10.1111/j.1749-6632.1973.tb20484.x.
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Binding of adrenergic beta-receptor antagonists to human serum albumin.肾上腺素能β受体拮抗剂与人血清白蛋白的结合
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Drug-albumin binding.药物-白蛋白结合
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Quantitation in plasma and urine of acebutolol and a major metabolite with preliminary observations on their disposition kinetics in man.醋丁洛尔及其主要代谢产物在血浆和尿液中的定量分析以及对其在人体处置动力学的初步观察。
Res Commun Chem Pathol Pharmacol. 1976 Sep;15(1):31-51.
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Acebutolol disposition after intravenous administration.静脉注射后醋丁洛尔的处置情况。
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Equilibrium dialysis: a new approach.平衡透析:一种新方法。
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Evaluation of methods to determine protein-binding of drugs. Equilibrium dialysis, ultrafiltration, ultracentrifugation, gel filtration.药物蛋白结合测定方法的评估。平衡透析、超滤、超速离心、凝胶过滤。
Arzneimittelforschung. 1977 Jul;27(7):1373-80.
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A randomized crossover comparison of acebutolol and methyldopa in the treatment of mild to moderate essential hypertension.
Curr Med Res Opin. 1978;5(9):675-81. doi: 10.1185/03007997809110206.
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Increased plasma protein binding of propranolol and chlorpromazine mediated by disease-induced elevations of plasma alpha1 acid glycoprotein.
N Engl J Med. 1978 Dec 28;299(26):1435-9. doi: 10.1056/NEJM197812282992604.
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Suppression of premature ventricular contractions by acebutolol.
Circulation. 1977 May;55(5):785-91. doi: 10.1161/01.cir.55.5.785.